Marine Drugs最新文献

{"title":"The Invertebrate-Derived Antimicrobial Peptide Cm-p5 Induces Cell Death and ROS Production in Melanoma Cells.","authors":"Ernesto M Martell-Huguet, Daniel Alpízar-Pedraza, Armando Rodriguez, Marc Zumwinkel, Mark Grieshober, Fidel Morales-Vicente, Ann-Kathrin Kissmann, Markus Krämer, Steffen Stenger, Octavio L Franco, Ludger Ständker, Anselmo J Otero-Gonzalez, Frank Rosenau","doi":"10.3390/md23070273","DOIUrl":"https://doi.org/10.3390/md23070273","url":null,"abstract":"<p><p>Nowadays, healthcare systems face two global challenges: the rise of multidrug-resistant pathogens and the growing incidence of cancer. Due to their broad spectrum of activities, antimicrobial peptides emerged as potential alternatives against both threats. Our group previously described the antifungal activity of the α-helical peptide Cm-p5, a derivative of the natural peptide Cm-p1, isolated from the coastal mollusk <i>Cenchritis muricatus</i>; however, its anti-cancer properties remained unexplored. Analyses through calorimetry and molecular dynamics simulations suggest the relevance of phosphatidylserine for the attachment of Cm-p5 to cancer cell membranes. Cm-p5 exhibited cytotoxic activity in a dose-dependent manner against A375 melanoma cells, without toxicity against non-malignant cells or hemolytic activity. DAPI/PI and DiSC3(5) staining confirmed permeabilization, disruption, and depolarization of A375 cytoplasmic membranes by Cm-p5. Furthermore, Annexin V-FITC/PI assay revealed the induction of cellular death in melanoma cells, which can result from the cumulative membrane damage and oxidative stress due to the overproduction of reactive oxygen species (ROS). Moreover, after the treatment, the proliferation of A375 cells was dampened for several days, suggesting that Cm-p5 might inhibit the recurrence of melanomas. These findings highlight the multifunctional nature of Cm-p5 and its potential for treating malignant melanoma.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144708010","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Sequential Extraction of Bioactive Saponins from <i>Cucumaria frondosa</i> Viscera: Supercritical CO₂-Ethanol Synergy for Enhanced Yields and Antioxidant Performance.","authors":"Jianan Lin, Guangling Jiao, Azadeh Kermanshahi-Pour","doi":"10.3390/md23070272","DOIUrl":"https://doi.org/10.3390/md23070272","url":null,"abstract":"<p><p>This study investigates the sequential extraction of lipids and saponins from <i>C. frondosa</i> viscera. Lipids were extracted using supercritical carbon dioxide (scCO₂) in the presence of ethanol (EtOH) as a co-solvent. Subsequently, the lipid-extracted viscera underwent three saponin extraction approaches, scCO₂-scCO₂, scCO₂-EtOH, and scCO₂-hot water, resulting in saponin-rich extracts. Process parameter investigation for saponin extraction from scCO₂-defatted viscera revealed minimal effects of temperature, pressure, extraction time, static extraction, and EtOH concentration on saponin yields, allowing for milder operational conditions (35 °C, 20 MPa, 30 min dynamic extraction, 75% EtOH at 0.5 mL/min) to achieve energy-efficient recovery. Continuous EtOH feeding predominates the scCO₂ extraction of saponins. The sequential scCO₂ extraction of lipid and saponins yielded saponins at 9.13 mg OAE/g, while scCO₂ extraction of lipid followed by a 24 h 70% EtOH extraction of saponins achieved 16.26 mg OAE/g, closely matching the optimized ultrasonic-assisted extraction of saponins (17.31 mg OAE/g) from hexane-defatted samples. Antioxidant activities of saponin-rich extracts obtained in the sequential scCO₂-EtOH extraction (17.12 ± 4.20% DPPH scavenging) and the sequential scCO₂-scCO₂ extraction (16.14 ± 1.98%) were comparable to BHT (20.39 ± 0.68%), surpassing that of hexane-defatted ultrasonic extracts (8.11 ± 1.16%). The optimized scCO₂-EtOH method offers a sustainable alternative, eliminating toxic solvents while maintaining high saponin yields and bioactivity.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144708007","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Greener Extraction Solutions for Microalgal Compounds.","authors":"Gwendoline Kopp, Chiara Lauritano","doi":"10.3390/md23070269","DOIUrl":"https://doi.org/10.3390/md23070269","url":null,"abstract":"<p><p>Conventional methods for extracting bioactive compounds from microalgae rely on organic solvents that are both polluting and potentially harmful to human health. In recent years, a noticeable shift has emerged toward greener extraction alternatives that are more environmentally friendly and sustainable. This review highlights various green extraction techniques, compounds, and yields obtained from different microalgal species for a range of applications and provides a comparison between the yields of conventional and green extraction methods. Green extraction methods have shown yields that are comparable to, or even exceed, those of conventional techniques, although they are predominantly studied for the extraction of lipids and pigments. This review aims to provide an overview of the current state of green extraction applied to microalgae, and to outline future research perspectives in this emerging field.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707994","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Fresh Perspective on Cyanobacterial Paralytic Shellfish Poisoning Toxins: History, Methodology, and Toxicology.","authors":"Zacharias J Smith, Kandis M Arlinghaus, Gregory L Boyer, Cathleen J Hapeman","doi":"10.3390/md23070271","DOIUrl":"https://doi.org/10.3390/md23070271","url":null,"abstract":"<p><p>Paralytic shellfish poisoning toxins (PSPTs) are a class of neurotoxins most known for causing illness from consuming contaminated shellfish. These toxins are also present in freshwater systems with the concern that they contaminate drinking and recreational waters. This review provides (1) a complete list of the 84+ known PSPTs and important chemical features; (2) a complete list of all environmental freshwater PSPT detections; (3) an outline of the certified PSPT methods and their inherent weaknesses; and (4) a discussion of PSPT toxicology, the weaknesses in existing data, and existing freshwater regulatory limits. We show ample evidence of production of freshwater PSPTs by cyanobacteria worldwide, but data and method uncertainties limit a proper risk assessment. One impediment is the poor understanding of freshwater PSPT profiles and lack of commercially available standards needed to identify and quantify freshwater PSPTs. Further constraints are the limitations of toxicological data derived from human and animal model exposures. Unassessed mouse toxicity data from 1978 allowed us to calculate and propose toxicity equivalency factors (TEF) for 11-hydroxysaxitoxin (11-OH STX; M2) and 11-OH dcSTX (dcM2). TEFs for the 11-OH STX epimers were calculated to be 0.4 and 0.6 for 11α-OH STX (M2α) and 11β-OH STX (M2β), while we estimate that TEFs for 11α-OH dcSTX (dcM2α) and 11β-OH dcSTX (dcM2β) congeners would be 0.16 and 0.23, respectively. Future needs for freshwater PSPTs include increasing the number of reference materials for environmental detection and toxicity evaluation, developing a better understanding of PSPT profiles and important environmental drivers, incorporating safety factors into exposure guidelines, and evaluating the accuracy of the established no-observed-adverse-effect level.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707980","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"From Sea to Relief: The Therapeutic Potential of Marine Algal Antioxidants in Pain Alleviation.","authors":"Mariola Belda-Antolí, Francisco A Ros Bernal, Juan Vicente-Mampel","doi":"10.3390/md23070270","DOIUrl":"https://doi.org/10.3390/md23070270","url":null,"abstract":"<p><p>Chronic pain affects approximately 20% of the global adult population, posing significant healthcare and economic challenges. Effective management requires addressing both biological and psychosocial factors, with emerging therapies such as antioxidants and marine algae offering promising new treatment avenues. Marine algae synthesize bioactive compounds, including polyphenols, carotenoids, and sulfated polysaccharides, which modulate oxidative stress, inflammation, and neuroimmune signaling pathways implicated in pain. Both preclinical and clinical studies support their potential application in treating inflammatory, neuropathic, muscular, and chronic pain conditions. Notable constituents include polyphenols, carotenoids (such as fucoxanthin), vitamins, minerals, and sulfated polysaccharides. These compounds modulate oxidative stress and inflammatory pathways, particularly by reducing reactive oxygen species (ROS) and downregulating cytokines such as tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Brown and red algae produce phlorotannins and fucoidans that alleviate pain and inflammation in preclinical models. Carotenoids like fucoxanthin demonstrate neuroprotective effects by influencing autophagy and inflammatory gene expression. Algal-derived vitamins (C and E) and minerals (magnesium, selenium, and zinc) contribute to immune regulation and pain modulation. Additionally, sulfated polysaccharides suppress microglial activation in the central nervous system (CNS). Marine algae represent a promising natural source of bioactive compounds with potential applications in pain management. Although current evidence, primarily derived from preclinical studies, indicates beneficial effects in various pain models, further research is necessary to confirm their efficacy, safety, and mechanisms in human populations. These findings advocate for the continued exploration of marine algae as complementary agents in future therapeutic strategies.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Diversity and Novelty of Venom Peptides in Vermivorous Cone Snails, Subgenus <i>Rhizoconus</i> (Gastropoda: Mollusca).","authors":"Christine Marie C Florece, Quentin Kaas, Neda Barghi, Arturo O Lluisma","doi":"10.3390/md23070266","DOIUrl":"https://doi.org/10.3390/md23070266","url":null,"abstract":"<p><p>A large majority of cone snails (a species in the genus <i>Conus</i>) are vermivorous (worm-hunting), but the diversity and bioactivity of their venom peptides remain largely unexplored. In this study, we report the first venom gland transcriptomes from two species in the <i>Rhizoconus</i> clade, <i>Conus capitaneus</i> and <i>Conus mustelinus</i>, and a new <i>Conus miles</i> transcriptome from a specimen collected in the Philippines. From the set of assembled sequences, a total of 225 <i>C. capitaneus</i>, 121 <i>C. miles</i>, and 168 <i>C. mustelinus</i> putative peptide toxin transcripts were identified, which were assigned to 27 canonical gene superfamilies in <i>C. capitaneus</i> and 24 in <i>C. miles</i> and in <i>C. mustelinus</i>. Most of these venom peptides are novel, and some exhibit new cysteine patterns. Clustering also revealed 12 putative novel gene superfamilies, highlighting the diversity of uncharacterized venom peptides in this group. The O1-, M-, O2-, and con-ikot-ikot superfamilies were the most abundant, while gene superfamilies such as D and G2 were highly expressed. Several hormone-like conopeptides were also identified in this study, revealing the vast diversity of conopeptides from the <i>Rhizoconus</i> species.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Characterization of Novel ACE-Inhibitory Peptides from <i>Nemopilema nomurai</i> Jellyfish Venom Hydrolysate: In Vitro and In Silico Approaches.","authors":"Ramachandran Loganathan Mohan Prakash, Deva Asirvatham Ravi, Du Hyeon Hwang, Changkeun Kang, Euikyung Kim","doi":"10.3390/md23070267","DOIUrl":"https://doi.org/10.3390/md23070267","url":null,"abstract":"<p><p>The venom of <i>Nemopilema nomurai</i> jellyfish represents a promising source of bioactive compounds with potential pharmacological applications. In our previous work, we identified two novel angiotensin-converting enzyme (ACE)-inhibitory peptides-IVGRPLANG (896.48 Da) and IGDEPRHQYL (1227.65 Da)-isolated from <i>N. nomurai</i> venom hydrolysates via papain digestion. In this study, we conducted a detailed biochemical and computational characterization of these peptides. The IC₅₀ values were determined to be 23.81 µM for IVGRPLANG and 5.68 µM for IGDEPRHQYL. Kinetic analysis using Lineweaver-Burk plots revealed that both peptides act as competitive ACE inhibitors, with calculated inhibition constants (K_i) of 51.38 µM and 5.45 µM, respectively. To assess the structural stability of the ACE-peptide complexes, molecular dynamics simulations were performed. Root mean square deviation (RMSD) and root mean square fluctuation (RMSF) analyses provided insights into complex stability, while interaction fraction analysis elucidated key bond types and residue-ligand contacts involved in binding. Furthermore, a network pharmacology approach was employed to predict therapeutic targets within the renin-angiotensin-aldosterone system (RAAS). Eleven target proteins were identified: IVGRPLANG was associated with REN, ACE, CTSB, CTSS, and AGTR2; IGDEPRHQYL was linked to REN, AGT, AGTR1, AGTR2, KNG1, and BDKR2. Molecular docking analyses using HADDOCK software (version 2.4) were conducted for all targets to evaluate binding affinities, providing further insight into the peptides' therapeutic potential.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Selective Antiproliferative Effects of Marine Oils on Neuroblastoma Cells in 3D Cultures.","authors":"Luís Freiría-Martínez, Jose María Oliva-Montero, Ainhoa Rodríguez-Tébar, Ola Hermanson, Santiago P Aubourg, Carlos Spuch, Isabel Medina","doi":"10.3390/md23070268","DOIUrl":"https://doi.org/10.3390/md23070268","url":null,"abstract":"<p><p>Dietary marine lipids enriched in <i>ω-3</i> polyunsaturated fatty acids (PUFAs) are spotlighted for favorable effects in neurodegenerative conditions and tumor cell proliferation. Commercial marine oils, with high EPA and DHA content, consist of non-polar lipids constituted by triacylglycerols or polar oils composed of phospholipids. Both classes have shown different activities to significantly inhibit proliferation and migration, and induce apoptosis in cancer cells. This work was aimed at testing marine oils' associated effects on neuroblastoma (NB) and glioblastoma (GB). Commercial non-polar and polar marine oils were studied in 3D spheroid models developed with human neuroblastoma, GB, and non-nervous embryonic kidney cell lines. This study also included results provided by a new sustainable polar marine oils source: fishery side-streams. Cell viability and mitochondrial activity assessments demonstrated that both marine oils dramatically reduced NB cells' metabolism, proliferation, and viability. Effects on GB and epithelial cells were different, including a metabolic increase. Marine oils also induce cell differentiation and selectively modulate the activity of neurons and glia, depending on the oils' chemical form. Sustainable polar oil showed bioactive characteristics similar to commercial krill oil. We propose that marine oils rich in triacylglycerols and phospholipids with high EPA and DHA levels may be a useful tool in NB antiproliferative therapies.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144708006","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cladolosides of Groups S and T: Triterpene Glycosides from the Sea Cucumber <i>Cladolabes schmeltzii</i> with Unique Sulfation; Human Breast Cancer Cytotoxicity and QSAR.","authors":"Alexandra S Silchenko, Elena A Zelepuga, Ekaterina A Chingizova, Ekaterina S Menchinskaya, Kseniya M Tabakmakher, Anatoly I Kalinovsky, Sergey A Avilov, Roman S Popov, Pavel S Dmitrenok, Vladimir I Kalinin","doi":"10.3390/md23070265","DOIUrl":"https://doi.org/10.3390/md23070265","url":null,"abstract":"&lt;p&gt;&lt;p&gt;Four new minor monosulfated triterpene penta- and hexaosides, cladolosides S (&lt;b&gt;1&lt;/b&gt;), S&lt;sub&gt;1&lt;/sub&gt; (&lt;b&gt;2&lt;/b&gt;), T (&lt;b&gt;3&lt;/b&gt;), and T&lt;sub&gt;1&lt;/sub&gt; (&lt;b&gt;4&lt;/b&gt;), were isolated from the Vietnamese sea cucumber &lt;i&gt;Cladolabes schmeltzii&lt;/i&gt; (Sclerodactylidae, Dendrochirotida). The structures of the compounds were established based on extensive analysis of 1D and 2D NMR spectra as well as HR-ESI-MS data. Cladodosides S (&lt;b&gt;1&lt;/b&gt;), S&lt;sub&gt;1&lt;/sub&gt; (&lt;b&gt;2&lt;/b&gt;) and T (&lt;b&gt;3&lt;/b&gt;), T&lt;sub&gt;1&lt;/sub&gt; (&lt;b&gt;4&lt;/b&gt;) are two pairs of dehydrogenated/hydrogenated compounds that share identical carbohydrate chains. The oligosaccharide chain of cladolosides of the group S is new for the sea cucumber glycosides due to the presence of xylose residue attached to C-4 Xyl1 in combination with a sulfate group at C-6 MeGlc4. The oligosaccharide moiety of cladolosides of the group T is unique because of the position of the sulfate group at C-3 of the terminal sugar residue instead of the 3&lt;i&gt;-O&lt;/i&gt;-Me group. This suggests that the enzymatic processes of sulfation and &lt;i&gt;O&lt;/i&gt;-methylation that occur during the biosynthesis of glycosides can compete with each other. This can presumably occur due to the high level of expression or activity of the enzymes that biosynthesize glycosides. The mosaicism of glycoside biosynthesis (time shifting or dropping out of some biosynthetic stages) may indicate a lack of compartmentalization inside the cells of organism producers, leading to a certain degree of randomness in enzymatic reactions; however, this also offers the advantage of providing chemical diversity of the glycosides. Analysis of the hemolytic activity of a series of 26 glycosides from &lt;i&gt;C. schmeltzii&lt;/i&gt; revealed some patterns of structure-activity relationships: the presence or absence of 3&lt;i&gt;-O&lt;/i&gt;-methyl groups has no significant impact, hexaosides, which are the final products of biosynthesis and predominant compounds of the glycosidic fraction of &lt;i&gt;C. schmeltzii&lt;/i&gt;, are more active than their precursors, pentaosides, and the minor tetraosides, cladolosides of the group A, are weak membranolytics and therefore are not synthesized in large quantities. Two glycosides from &lt;i&gt;C. schmeltzii&lt;/i&gt;, cladolosides D (&lt;b&gt;18&lt;/b&gt;) and H&lt;sub&gt;1&lt;/sub&gt; (&lt;b&gt;26&lt;/b&gt;), display selectivity of cytotoxic action toward triple-negative breast cancer cells MDA-MB-231, while remaining non-toxic in relation to normal mammary cells MCF-10A. Quantitative structure-activity relationships (QSAR) were calculated based on the correlational analysis of the physicochemical properties and structural features of the glycosides and their hemolytic and cytotoxic activities against healthy MCF-10A cells and cancer MCF-7 and MDA-MB-231 cell lines. QSAR highlighted the complexity of the relationships as the cumulative effect of many minor contributions from individual descriptors can have a significant impact. Furthermore, many structural elements were found to have different effects on the activity of the glycoside","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707987","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lipotrichaibol A and Trichoderpeptides A-D: Five New Peptaibiotics from a Sponge-Derived <i>Trichoderma</i> sp. GXIMD 01001.","authors":"Weichan Yang, Zhenzhou Tang, Xiaowei Luo, Yuman Gan, Meng Bai, Houwen Lin, Chenghai Gao, Ling Chai, Xiao Lin","doi":"10.3390/md23070264","DOIUrl":"https://doi.org/10.3390/md23070264","url":null,"abstract":"<p><p>Five previously undescribed peptaibiotics, including one 7-mer lipopeptaibol named lipotrichaibol A (<b>1</b>), and four 11-mer peptaibiotics named trichoderpeptides A-D (<b>2</b>-<b>5</b>) were isolated from the rice culture medium of the sponge-derived fungus <i>Trichoderma</i> sp. GXIMD 01001. Their structures and absolute configurations were unambiguously established by extensive spectroscopic data analysis and advanced Marfey's method. All isolated compounds were evaluated via CCK8 bioassays to investigate their antiproliferative activity. Only compound <b>1</b> exerted potent cytotoxicity against HT-29 and DLD-1 cells with IC₅₀ values at 10.3 ± 1.9 and 12.31 ± 1.5 μM, respectively. In further in vitro bioassay, compound <b>1</b> exhibited significant inhibition in colony formation assay, induced apoptosis and blocked the cell cycle in the G0/G1 phase. The mechanism may be related to the regulation of the Erk1/2 signaling pathway.</p>","PeriodicalId":18222,"journal":{"name":"Marine Drugs","volume":"23 7","pages":""},"PeriodicalIF":4.9,"publicationDate":"2025-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707997","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}